59525-14-3Relevant academic research and scientific papers
Synthesis, in silico study and cholinesterases inhibition activity of 2-substituted 2, 3-dihydroquinazolin-4(1H)-one derivatives
Sarfraz, Muhammad,Sultana, Nargis,Jamil, Muhammad,Tariq, Muhammad Ilyas
, p. 227 - 234 (2018/08/03)
We have synthesized and evaluated a number of 2, 3-dihydroquinazolin-4(1H)-one derivatives as inhibitors of cholinesterases. In vitro assay results revealed that all synthesized compounds are active against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes and few compounds having longer alkyl chain at C-2 position showed better inhibition activity than standard drug galantamine. Moreover, bromo derivatives 6a-d were more active than nitro 5a-d and their un-substituted counterparts 4a-d. Amongst all, compound 6d, with IC50 values of 4.8±1.01 μM (AChE) and 11.1±1.15 μM (BChE) can be considered as good cholinesterase (AChE/BChE), inhibitor with greater selectivity towards BChE. In silico calculations revealed that all compounds have good pharmacokinetic profile along with having high probabilities for penetration across blood brain barrier (BBB), human intestinal absorption (HIA), non-AMES toxicity and non-carcinogenicity except nitro substituted derivatives which were predicted to show AMES toxicity. The synthesized compounds may lead toward development of new potent cholinesterase inhibitors.
2-propyl-4-chloriquine oxazoline derivatives and its preparation method and application
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Paragraph 0054-0056, (2017/02/28)
The invention relates to a 2-propyl-4-chloroquinazoline derivative, its preparation method thereof and its application thereof, and provides a compound with a structure shown as a general formula (I) which is defined as a specification. The compound has good antineoplastic activity, and is expected to be exploited to a targeted drug for treating tumor.
Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds
Segarra, Victor,Crespo, M. Isabel,Pujol, Ferran,Beleta, Jorge,Domenech, Teresa,Miralpeix, Montserrat,Palacios, Jose M.,Castro, Ana,Martinez, Ana
, p. 505 - 510 (2007/10/03)
A 4-centre PDE 4 pharmacophore search has been carried out in several 3D-databases containing compounds belonging to different therapeutic areas. Losartan, an angiotensin-II antagonist, has been identified as a new lead compound for developing PDE 4 inhibitors. New families of compounds derived from losartan has been synthesized and their PDE inhibition has been measured.
